Patents Examined by Emily A Bernhardt
  • Patent number: 11352344
    Abstract: Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds of formula (Ia), which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: June 7, 2022
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Darren W. Engers, Kayla J. Temple
  • Patent number: 11319303
    Abstract: It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators.
    Type: Grant
    Filed: May 18, 2018
    Date of Patent: May 3, 2022
    Inventors: Cheng Luo, Yuli Xie, Bing Zhou, Zhiyi Yao, Liyan Yue, Wei Wan, Bidong Zhang, Yuanyuan Zhang, Hualiang Jiang, Kaixian Chen
  • Patent number: 11319286
    Abstract: The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof, has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.
    Type: Grant
    Filed: August 2, 2018
    Date of Patent: May 3, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tatsuhiko Fujimoto, Kentaro Rikimaru, Koichiro Fukuda, Hiromichi Sugimoto, Takahiro Matsumoto, Yuichi Kajita, Satoshi Mikami, Yuhei Miyanohana, Tatsuki Koike, Masaki Daini, Masaki Ogino, Kohei Takeuchi, Tohru Miyazaki, Yoshiteru Ito, Norihito Tokunaga, Takahiro Sugimoto, Tsuneo Oda, Yasutaka Hoashi, Yasushi Hattori, Keisuke Imamura
  • Patent number: 11312693
    Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4 alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as oste
    Type: Grant
    Filed: July 27, 2020
    Date of Patent: April 26, 2022
    Assignee: Medivir AB
    Inventors: Lourdes Salvador Oden, Magnus Nilsson, Pia Kahnberg, Bertil Samuelsson, Urszula Grabowska
  • Patent number: 11306071
    Abstract: 5,6-disubstituted 2-aminopyrazine compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in oncology.
    Type: Grant
    Filed: January 17, 2020
    Date of Patent: April 19, 2022
    Assignee: Nuvation Bio Inc.
    Inventors: Son Minh Pham, Jayakanth Kankanala, Pradeep S. Jadhavar, Baban Mohan Mulik, Farha Khan, Sreekanth A. Ramachandran
  • Patent number: 11306101
    Abstract: Provided herein are 1-oxo-isoindoline-5-carboxamide compounds having the following structure: wherein R1, R2, R3, R4 and n are as defined herein, compositions comprising an effective amount of a 1-oxo-isoindoline-5-carboxamide compound, and methods for treating or preventing disorders.
    Type: Grant
    Filed: May 29, 2020
    Date of Patent: April 19, 2022
    Assignee: Celgene Corporation
    Inventors: Frans Baculi, Katherine Northcote, Matthew D. Correa, Joshua Hansen, Laurie A. Lebrun, Chin-Chun Lu, Gang Lu, Mark A. Nagy, Sophie Peng, Sophie Perrin-Ninkovic
  • Patent number: 11274093
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, isotopic form, stereoisomer or prodrug thereof, wherein A, B, X, R1, R2a, R2b, R2c, L, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: January 24, 2018
    Date of Patent: March 15, 2022
    Inventors: Liansheng Li, Jun Feng, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
  • Patent number: 11261158
    Abstract: The present disclosure relates to a preparation method of methyl (E)-1-acetyl-3-(methoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate from methyl 2-oxoindoline-6-carboxylate using high reaction temperatures and a reaction solvent enabling azeotropic removal of acetic acid during the reaction.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: March 1, 2022
    Assignee: FERMION OY
    Inventors: Antti Piisola, Jan Tois
  • Patent number: 11261200
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.
    Type: Grant
    Filed: October 5, 2017
    Date of Patent: March 1, 2022
    Assignee: The Global Alliance for TB Drug Development, Inc.
    Inventors: Takushi Kaneko, Nader Fotouhi
  • Patent number: 11254665
    Abstract: The present application relates to a crystalline sulfamide compound, and in particular relates to a crystalline (S)—N—((S)-1-(2-chlorphenyl)-2-((3,3-difluorocyclobutyl)amido)-2oxoethyl)-2-(4-cyanopyridin-2-base)-N-(3-fluorophenyl)-isothiazolidine-3-formamide 1,1-dioxide, and a preparation method therefor, a crystalline composition, a pharmaceutical composition and uses thereof. An X-ray powder diffraction spectrum of a crystalline hydrate of formula II of the present application has diffraction peaks at positions of about 14.40°, 20.28°, 20.94°, 22.02°, and 24.46°, represented by 2?. The crystalline hydrate of formula II of the present application has good IDH1 inhibitory activity and performs high stability, and therefore has advantages in physical property, safety and metabolic stability, and has high medicine value.
    Type: Grant
    Filed: September 21, 2018
    Date of Patent: February 22, 2022
    Inventors: Xiquan Zhang, Wenwei Xu, Mingming Li, Minmin Kong, Shufeng Wu, Aiming Zhang
  • Patent number: 11248013
    Abstract: The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.
    Type: Grant
    Filed: October 28, 2019
    Date of Patent: February 15, 2022
    Assignee: Rakovina Therapeutics Inc.
    Inventors: Wang Shen, Jack Maung, Aimin Zhang, Xiaoling Zheng
  • Patent number: 11247982
    Abstract: The present invention relates to the field of prevention and treatment of diseases involving NMDA receptors of the central nervous system. It relates more specifically to compounds of 1-(indol-3-yl)-3-hydroxy-3-(2-oxo-2-ethyl)-indol-2-ones type, as a drug, and the use of such compounds in the preparation of pharmaceutical compositions. These pharmaceutical compositions may in particular be intended to prevent or treat diseases involving NMDA receptors of the central nervous system, in particular severe/resistant epilepsy and cognitive disorders resulting therefrom, especially autism, but also strokes, schizophrenia, degenerative diseases involving the activation of NMDA receptors, such as Parkinson's disease and Alzheimer's disease, Rett syndrome, or amyotrophic lateral sclerosis, migraine, dementia and major depressive disorder.
    Type: Grant
    Filed: May 29, 2018
    Date of Patent: February 15, 2022
    Assignee: ADPUERIVITAM
    Inventors: Mouad Alami, Jean Daniel Brion, Samir Messaoudi, Sabrina Touchet, Gilles Galvani, Olivier Dulac, Svetlana Gataullina, Caroline Nous
  • Patent number: 11247985
    Abstract: The present invention is directed to methods of inhibiting p97 and compounds and compositions useful in such methods. Diseases and conditions the can be treated with the compounds and compositions of the invention include, but are not limited to, cancer and neurodegenerative disorders susceptible to treatment by inhibition of p97.
    Type: Grant
    Filed: January 21, 2020
    Date of Patent: February 15, 2022
    Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, National Institutes of Health, A Component of the U.S. Department of Hearth and Human Services, The Regents of the University of California
    Inventors: Donna M. Huryn, Peter Wipf, Matthew G. LaPorte, Raffaele Colombo, Marina Kovaliov, Chaemin Lim, Celeste Natalie Alverez, Zhizhou Yue, Lalith Palitha Samankumara, Alexander Julian Chatterley, Yongzhao Yan, Mary Liang, Neal J. Green, Eric T. Baldwin, William J. Moore, Michelle Arkin, R. Jeffrey Neitz, Kean-Hooi Ang, Clifford Bryant, Stacie Bulfer
  • Patent number: 11242335
    Abstract: A class of fluorine-substituted indazole compounds and uses thereof having the general formula depicted below in which C1 is where is the bond through which C1 is attached to L, and C2 is where is the bond through which C2 is attached to indazole, and pharmaceutical compositions containing these compounds. The compounds and pharmaceutical compositions of the invention can be used as soluble guanylate cyclase simulators.
    Type: Grant
    Filed: April 10, 2018
    Date of Patent: February 8, 2022
    Inventors: Yinglin Zuo, Xiaojun Wang, Chuanwen Yang, Jiancheng Wang, Shengtian Cao, Fangyuan Wu, Yingjun Zhang, Siegfried Goldmann
  • Patent number: 11236083
    Abstract: The present invention provides compounds of Formula (I) which can be used as SGK inhibitors; pharmaceutical compositions comprising the compounds of the invention; as well as uses and methods for treating a disease mediated by SGK by administering the compounds of the invention.
    Type: Grant
    Filed: November 24, 2017
    Date of Patent: February 1, 2022
    Inventor: Jun Xian
  • Patent number: 11236093
    Abstract: The present invention relates to a compound suitable for use as a kinase inhibitor according to general formula (I) [compound (C), herein after], or the N-oxide, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or stereoisomer thereof, formula (I) wherein A, R1, R2, R3, R3?, R4, R4?, X, Y, Z, T are as defined in the claims. The invention further relates to an in vitro method of inhibiting protein kinase activity which comprises contacting a protein kinase with a compound of formula (I), or the N-oxide, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or stereoisomer thereof. The invention further relates to the compounds of formula (I) per se, as well as to their use as a medicament, and for use or in a method of treatment of a disease mediated by a protein kinase selected from cancer, inflammatory disorders, cardiovascular diseases, viral induced diseases, circulatory diseases, fibro-proliferative diseases and pain sensitization disorders.
    Type: Grant
    Filed: May 4, 2017
    Date of Patent: February 1, 2022
    Assignee: B.C.I. Pharma
    Inventors: Dominique Surleraux, Claire Amiable, Rémi Guillon
  • Patent number: 11236066
    Abstract: The present invention provides novel crystalline forms of niraparib tosylate. Specific crystalline forms provided by the present invention include niraparib tosylate Form APO-I, a co-crystal of niraparib tosylate and urea, and niraparib tosylate Form APO-II, a co-crystal of niraparib tosylate and oxalic acid. Also provided are pharmaceutical compositions including the niraparib tosylate crystalline forms, and the use of these forms in treatment or prevention of conditions which can be ameliorated by the inhibition of poly(ADP-ribose) polymerase (PARP), in particular certain forms of cancer.
    Type: Grant
    Filed: July 14, 2020
    Date of Patent: February 1, 2022
    Assignee: Apotex Inc.
    Inventors: Alexander J. Stirk, Fabio E. S. Souza, Avedis Karadeolian, Allan W. Rey
  • Patent number: 11229648
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: July 21, 2020
    Date of Patent: January 25, 2022
    Assignee: Novartis AG
    Inventors: Atwood Kim Cheung, Donovan Noel Chin, Natalie Dales, Aleem Fazal, Timothy Brian Hurley, John Kerrigan, Gary O'Brien, Lei Shu, Robert Sun, Moo Je Sung
  • Patent number: 11225482
    Abstract: The present invention provides novel compounds having the general formula: wherein R1, R2, A and X are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: January 18, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Zhanling Cheng, Xingchun Han, Min Jiang, Song Yang
  • Patent number: 11220503
    Abstract: The present invention provides a compound of formula I, a cis-trans isomer, an enantiomer, a diastereoisomer, a racemate, a solvate, a hydrate, or a pharmaceutical acceptable salt and ester thereof, a preparation method for preparing the same, a pharmaceutical composition comprising the same and a use of the compound as an ?5-GABAA receptor regulator, wherein T, Z, A and Y are as defined in the description.
    Type: Grant
    Filed: December 8, 2016
    Date of Patent: January 11, 2022
    Assignee: Shanghai SIMR Biotech Co., Ltd.
    Inventors: Shuai Li, Yong Sun